NS-1619. Selective and Potent Enhancer of KCa1.1 Channels.
The large conductance voltage- and Ca2+-activated K+ (BK) channels, also known as BKCa, KCa1.1, Slo, or MaxiK, play an important role in modulating nerve and muscle cell contractility and excitability.
BK channels are activated by both depolarizing voltages and by an increase in intracellular free Ca2+, thus coupling the membrane potential to intracellular signaling.
NS-1619 is a potent and selective KCa1.1 channel modulator (enhancer). It has the potential to modulate cell excitability in neurons and smooth muscle. The effect of relaxation of NS-1619 on the BK channel in smooth muscle cells has an EC50 of 10�30 μM. It is also dose-dependent, resulting in a shift of the activation curve by up to -50 mV towards negative membrane potentials, but fully reversible.
Ion Channel Modulators; K+ Channel Openers
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